(19)
(11) EP 4 393 487 A3

(12) EUROPEAN PATENT APPLICATION

(88) Date of publication A3:
21.08.2024 Bulletin 2024/34

(43) Date of publication A2:
03.07.2024 Bulletin 2024/27

(21) Application number: 24159685.7

(22) Date of filing: 04.11.2015
(51) International Patent Classification (IPC): 
C07C 225/20(2006.01)
A61P 25/02(2006.01)
A61P 25/24(2006.01)
 A61K 31/215(2006.01)
A61P 25/22(2006.01)
A61P 25/28(2006.01)
(52) Cooperative Patent Classification (CPC):
C07B 2200/05; C07B 59/001; C07C 2601/14; A61K 45/06; A61K 9/2013; A61K 9/2027; A61K 9/2031; A61K 9/2054; A61K 31/135; C07C 225/20; A61K 9/2059; A61P 25/02; A61P 25/22; A61P 25/24; A61P 25/28
 
C-Sets:
A61K 31/135, A61K 2300/00;
(84) Designated Contracting States:
AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR

(30) Priority: 04.11.2014 US 201462074645 P

(62) Application number of the earlier application in accordance with Art. 76 EPC:
15856205.8 / 3215147

(71) Applicant: ACADIA Pharmaceuticals Inc.
San Diego, CA 92130 (US)

(72) Inventors:
  • NIVOROZHKIN, Alex
    West Roxbury, 02132 (US)
  • LANDRAU, Nelson
    Marlborough, 01752 (US)

(74) Representative: Maiwald GmbH 
Grünstraße 25
40212 Düsseldorf
40212 Düsseldorf (DE)

   


(54) NEURO-ATTENUATING KETAMINE AND NORKETAMINE COMPOUNDS, DERIVATIVES THEREOF, AND METHODS


(57) The present invention is directed to novel neuro-attentuating norketamine (NANKET) compounds according to any one of formulas (I - shown below), (I-A) and (I-B), or any of the compounds described in Tables A-D, or in any of the Examples provided herein, and pharmaceutically acceptable salts thereof, novel pharmaceutical formulations and novel methods of uses thereof. The present invention also features novel oral neuro-attenuating ketamine (NAKET) and neuro-attenuating norketamine (NANKET) modified-release pharmaceutical formulations, and novel methods of administration thereof, which ensure the steady release of a therapeutically effective amount of ketamine, norketamine, or derivatives thereof from the oral modified-release pharmaceutical formulations without neurologically toxic spikes in plasma concentration of the ketamine, norketamine, or derivatives during the release periods.









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